PH12016500989B1 - Crystalline salt of (s)-(2-(6-chloro-7-methyl-1h-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1 -yl)(5-methoxy-2-(2h-1,2,3-triazol-2-yl)phenyl)methanone as orexin receptor antagonists - Google Patents
Crystalline salt of (s)-(2-(6-chloro-7-methyl-1h-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1 -yl)(5-methoxy-2-(2h-1,2,3-triazol-2-yl)phenyl)methanone as orexin receptor antagonistsInfo
- Publication number
- PH12016500989B1 PH12016500989B1 PH12016500989A PH12016500989A PH12016500989B1 PH 12016500989 B1 PH12016500989 B1 PH 12016500989B1 PH 12016500989 A PH12016500989 A PH 12016500989A PH 12016500989 A PH12016500989 A PH 12016500989A PH 12016500989 B1 PH12016500989 B1 PH 12016500989B1
- Authority
- PH
- Philippines
- Prior art keywords
- methylpyrrolidin
- triazol
- imidazol
- benzo
- chloro
- Prior art date
Links
- 229940123730 Orexin receptor antagonist Drugs 0.000 title abstract 2
- NBGABHGMJVIVBW-QHCPKHFHSA-N [(2s)-2-(5-chloro-4-methyl-1h-benzimidazol-2-yl)-2-methylpyrrolidin-1-yl]-[5-methoxy-2-(triazol-2-yl)phenyl]methanone Chemical compound N1([C@](CCC1)(C)C=1NC2=CC=C(Cl)C(C)=C2N=1)C(=O)C1=CC(OC)=CC=C1N1N=CC=N1 NBGABHGMJVIVBW-QHCPKHFHSA-N 0.000 title 1
- 150000003839 salts Chemical class 0.000 title 1
- HJVGDXBEMFHGKI-BQAIUKQQSA-N [(2s)-2-(5-chloro-4-methyl-1h-benzimidazol-2-yl)-2-methylpyrrolidin-1-yl]-[5-methoxy-2-(triazol-2-yl)phenyl]methanone;hydrochloride Chemical compound Cl.N1([C@](CCC1)(C)C=1NC2=CC=C(Cl)C(C)=C2N=1)C(=O)C1=CC(OC)=CC=C1N1N=CC=N1 HJVGDXBEMFHGKI-BQAIUKQQSA-N 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4192—1,2,3-Triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Anesthesiology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IB2013060595 | 2013-12-03 | ||
| PCT/IB2014/066509 WO2015083071A1 (en) | 2013-12-03 | 2014-12-02 | Crystalline salt form of (s)-(2-(6-chloro-7-methyl-1 h-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1 -yl)(5-methoxy-2-(2h-1,2,3-triazol-2-yl)phenyl)methanone as orexin receptor antagonist |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| PH12016500989A1 PH12016500989A1 (en) | 2016-06-20 |
| PH12016500989B1 true PH12016500989B1 (en) | 2019-11-13 |
Family
ID=52282787
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PH12016500989A PH12016500989B1 (en) | 2013-12-03 | 2016-05-26 | Crystalline salt of (s)-(2-(6-chloro-7-methyl-1h-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1 -yl)(5-methoxy-2-(2h-1,2,3-triazol-2-yl)phenyl)methanone as orexin receptor antagonists |
Country Status (31)
| Country | Link |
|---|---|
| US (2) | US9790208B2 (de) |
| EP (1) | EP3077390B1 (de) |
| JP (1) | JP6091716B2 (de) |
| KR (1) | KR101839716B1 (de) |
| CN (1) | CN105793258B (de) |
| AU (1) | AU2014358743B2 (de) |
| CA (1) | CA2929720C (de) |
| CL (1) | CL2016001348A1 (de) |
| CY (1) | CY1119687T1 (de) |
| DK (1) | DK3077390T3 (de) |
| EA (1) | EA030109B1 (de) |
| ES (1) | ES2651508T3 (de) |
| HR (1) | HRP20171772T1 (de) |
| HU (1) | HUE034656T2 (de) |
| IL (1) | IL245922B (de) |
| LT (1) | LT3077390T (de) |
| MA (1) | MA39164B1 (de) |
| MX (1) | MX362701B (de) |
| MY (1) | MY176244A (de) |
| NO (1) | NO3077390T3 (de) |
| NZ (1) | NZ721493A (de) |
| PH (1) | PH12016500989B1 (de) |
| PL (1) | PL3077390T3 (de) |
| PT (1) | PT3077390T (de) |
| SA (1) | SA516371248B1 (de) |
| SG (1) | SG11201604541WA (de) |
| SI (1) | SI3077390T1 (de) |
| TW (1) | TWI636982B (de) |
| UA (1) | UA119151C2 (de) |
| WO (1) | WO2015083071A1 (de) |
| ZA (1) | ZA201604501B (de) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2617863T3 (es) | 2012-06-04 | 2017-06-20 | Actelion Pharmaceuticals Ltd. | Derivados de bencimidazol-prolina |
| MY179862A (en) | 2013-12-03 | 2020-11-18 | Idorsia Pharmaceuticals Ltd | Crystalline form of (s)-(2-(6-chloro-7-methyl-1h-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1 -yl)(5-methoxy-2-(2h-1,2,3-triazol-2-yl)phenyl)methanone and its use as orexin receptor antagonists |
| UA119151C2 (uk) * | 2013-12-03 | 2019-05-10 | Ідорсія Фармасьютікалз Лтд | КРИСТАЛІЧНА СОЛЬОВА ФОРМА (S)-(2-(6-ХЛОР-7-МЕТИЛ-1H-БЕНЗО[d]ІМІДАЗОЛ-2-ІЛ)-2-МЕТИЛПІРОЛІДИН-1-ІЛ)(5-МЕТОКСИ-2-(2H-1,2,3-ТРИАЗОЛ-2-ІЛ)ФЕНІЛ)МЕТАНОНУ ЯК АНТАГОНІСТ ОРЕКСИНОВОГО РЕЦЕПТОРА |
| SI3077391T1 (sl) | 2013-12-04 | 2018-11-30 | Idorsia Pharmaceuticals Ltd | Uporaba benzimidazol-prolinskih derivatov |
| LT3619199T (lt) | 2017-05-03 | 2021-09-27 | Idorsia Pharmaceuticals Ltd | 2-([1,2,3]triazol-2-il)-benzenkarboksirūgšties darinių gamyba |
| EP4138822A1 (de) | 2020-04-19 | 2023-03-01 | Idorsia Pharmaceuticals Ltd | Medizinische verwendung von daridorexant |
| CN115925699B (zh) * | 2022-02-25 | 2023-10-03 | 南京知和医药科技有限公司 | 具有镇痛活性的稠环化合物及其制备方法与用途 |
| CN117736193B (zh) * | 2023-12-19 | 2024-07-23 | 南京知和医药科技有限公司 | 一种氘代稠环化合物及其制备方法与用途 |
| ES3038762A1 (es) | 2024-04-12 | 2025-10-14 | Moehs Iberica Sl | Procedimiento de síntesis de ácido 5-metoxi-2-(2H-1,2,3-triazol-2yl)benzoico, sal sódica de dicho ácido como intermedio de síntesis y uso del ácido o de su sal en la preparación de daridorexant y ciertos intermedios en la síntesis del mismo |
| WO2025253419A1 (en) * | 2024-06-06 | 2025-12-11 | Msn Laboratories Private Limited, R&D Center | Solid state forms of (s)-(2-(5-chloro-4-methyl-1h-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2h-1,2,3-triazol-2-yl)phenyl)methanone hydrochloride and processes for preparation thereof |
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| WO2002044172A1 (en) | 2000-11-28 | 2002-06-06 | Smithkline Beecham P.L.C. | Morpholine derivatives as antagonists of orexin receptors |
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| WO2002089800A2 (en) | 2001-05-05 | 2002-11-14 | Smithkline Beecham P.L.C. | N-aroyl cyclic amine derivatives as orexin receptor antagonists |
| GB0115862D0 (en) | 2001-06-28 | 2001-08-22 | Smithkline Beecham Plc | Compounds |
| CZ20033437A3 (cs) * | 2001-06-28 | 2004-09-15 | Smithkline Beecham P.L.C. | N-Aroylové cyklické aminové deriváty jako antagonisté orexinového receptoru |
| GB0124463D0 (en) | 2001-10-11 | 2001-12-05 | Smithkline Beecham Plc | Compounds |
| GB0127145D0 (en) | 2001-11-10 | 2002-01-02 | Smithkline Beecham | Compounds |
| GB0130393D0 (en) | 2001-12-19 | 2002-02-06 | Smithkline Beecham Plc | Compounds |
| GB0130335D0 (en) | 2001-12-19 | 2002-02-06 | Smithkline Beecham Plc | Compounds |
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| GB0806536D0 (en) | 2008-04-10 | 2008-05-14 | Glaxo Group Ltd | Novel compounds |
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| WO2010060471A1 (en) | 2008-11-26 | 2010-06-03 | Glaxo Group Limited | Piperidine derivatives useful as orexin receptor antagonists |
| EP2358713A1 (de) | 2008-11-26 | 2011-08-24 | Glaxo Group Limited | Als orexinantagonisten wirkende imidazopyridazinderivate |
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| ES2617863T3 (es) | 2012-06-04 | 2017-06-20 | Actelion Pharmaceuticals Ltd. | Derivados de bencimidazol-prolina |
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| MY179862A (en) | 2013-12-03 | 2020-11-18 | Idorsia Pharmaceuticals Ltd | Crystalline form of (s)-(2-(6-chloro-7-methyl-1h-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1 -yl)(5-methoxy-2-(2h-1,2,3-triazol-2-yl)phenyl)methanone and its use as orexin receptor antagonists |
| UA119151C2 (uk) * | 2013-12-03 | 2019-05-10 | Ідорсія Фармасьютікалз Лтд | КРИСТАЛІЧНА СОЛЬОВА ФОРМА (S)-(2-(6-ХЛОР-7-МЕТИЛ-1H-БЕНЗО[d]ІМІДАЗОЛ-2-ІЛ)-2-МЕТИЛПІРОЛІДИН-1-ІЛ)(5-МЕТОКСИ-2-(2H-1,2,3-ТРИАЗОЛ-2-ІЛ)ФЕНІЛ)МЕТАНОНУ ЯК АНТАГОНІСТ ОРЕКСИНОВОГО РЕЦЕПТОРА |
| SI3077391T1 (sl) | 2013-12-04 | 2018-11-30 | Idorsia Pharmaceuticals Ltd | Uporaba benzimidazol-prolinskih derivatov |
-
2014
- 2014-02-12 UA UAA201607115A patent/UA119151C2/uk unknown
- 2014-12-02 DK DK14824108.6T patent/DK3077390T3/da active
- 2014-12-02 AU AU2014358743A patent/AU2014358743B2/en active Active
- 2014-12-02 EP EP14824108.6A patent/EP3077390B1/de active Active
- 2014-12-02 US US15/101,832 patent/US9790208B2/en active Active
- 2014-12-02 JP JP2016536106A patent/JP6091716B2/ja active Active
- 2014-12-02 PL PL14824108T patent/PL3077390T3/pl unknown
- 2014-12-02 NO NO14824108A patent/NO3077390T3/no unknown
- 2014-12-02 HR HRP20171772TT patent/HRP20171772T1/hr unknown
- 2014-12-02 ES ES14824108.6T patent/ES2651508T3/es active Active
- 2014-12-02 EA EA201600436A patent/EA030109B1/ru not_active IP Right Cessation
- 2014-12-02 SI SI201430453T patent/SI3077390T1/sl unknown
- 2014-12-02 MX MX2016007216A patent/MX362701B/es active IP Right Grant
- 2014-12-02 MA MA39164A patent/MA39164B1/fr unknown
- 2014-12-02 PT PT148241086T patent/PT3077390T/pt unknown
- 2014-12-02 MY MYPI2016701995A patent/MY176244A/en unknown
- 2014-12-02 LT LTEP14824108.6T patent/LT3077390T/lt unknown
- 2014-12-02 WO PCT/IB2014/066509 patent/WO2015083071A1/en not_active Ceased
- 2014-12-02 TW TW103141830A patent/TWI636982B/zh active
- 2014-12-02 NZ NZ721493A patent/NZ721493A/en unknown
- 2014-12-02 KR KR1020167017678A patent/KR101839716B1/ko active Active
- 2014-12-02 SG SG11201604541WA patent/SG11201604541WA/en unknown
- 2014-12-02 CN CN201480065749.2A patent/CN105793258B/zh active Active
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2016
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